Rovalpituzumab tesirine  (Synonyms: SC-002)

Rovalpituzumab tesirine (SC-002) is an antibody-drug conjugate (ADC) with anticancer effects. Rovalpituzumab tesirine contains a DLL3-targeting antibody Rovalpituzumab (HY-P99043) tethered to a cytotoxic agent pyrrolobenzodiazepine by means of a protease-cleavable linker. Rovalpituzumab tesirine can be used for the stduy of small cell lung cancer (SCLC)^[1].

Rovalpituzumab tesirine (0.01-10000 pM, 96 h) can effectively bind to mice DLL3 in KP1 cells (SCLC model) expressing mice DLL3, exhibiting potent killing effects and exerting cytotoxicity through internalization of PBD toxin^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rovalpituzumab tesirine (0.03, 0.1, 0.3 mg/kg, i.p. one dose) inhibites tumor growth in a dose-dependent manner in the SCLC mice model, and the 0.3 mg/kg group achieves complete remission, the anti-tumor effect is more significant when combines with anti-PD1^[2].
Rovalpituzumab tesirine (0.03 mg/kg, i.p once every four days) combines with anti-PD1 in the SCLC mice model leads to the infiltration and activation of CD8⁺ T cells in the tumor, up-regulates PD-L1 and MHC1, overcomes immunosuppression, and activates DC and STING pathways, exerting a synergistic anti-tumor effect^[2].
Rovalpituzumab tesirine (0.1 mg/kg, i.p. one dose) combines with anti-PD-1 in a SCLC mice model demonstrats that CD8⁺ T cells are key effector cells for efficacy^[2].
Rovalpituzumab tesirine (0.03 mg/kg, i.p. one dose) induces long-term antitumor immune memory in combination with anti-PD1 in a SCLC mice model^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1613313-09-9

[Rovalpituzumab tesirine]

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• [1]. Blackhall F, et al. Efficacy and Safety of Rovalpituzumab Tesirine Compared With Topotecan as Second-Line Therapy in DLL3-High SCLC: Results From the Phase 3 TAHOE Study. J Thorac Oncol. 2021 Sep;16(9):1547-1558.  [Content Brief]

  [2]. Vitorino P, et al. Rova-T enhances the anti-tumor activity of anti-PD1 in a murine model of small cell lung cancer with endogenous Dll3 expression. Transl Oncol. 2021 Jan;14(1):100883.  [Content Brief]